高效液相色谱法研究人体内兰索拉唑片药动学和生物等效性

Determination of Lansoprazole in Human Plasma by HPLC:Application to Bioequivalence and Pharmacokinetics Study

目的研究健康人口服兰索拉唑片后的药动学和生物等效性。方法19个健康受试者采用随机分组自身交叉对照试验设计,口服兰索拉唑片30mg后用HPLC法测定血浆中兰索拉唑浓度,以DAS软件计算其药动学参数和评价生物等效性。结果在选定的色谱条件下兰索拉唑与内标及血浆杂质分离良好,在20～2000ng·mL-1范围内线性良好。相对回收率>95.14%,日内和日间RSD<13.2%。兰索拉唑片受试制剂和参比制剂的主要药动学参数:Tmax分别为(2.45±0.47)h和(2.45±0.47)h,Cmax分别为(818.0±275.2)ng·mL-1和(859.3±311.3)ng·mL-1;t1/2分别为(2.24±0.89)h和(2.18±0.85)h;AUC0→12分别为(2405±1141)ng.h.mL-1和(2511±1351)ng.h.mL-1;用面积法(AUC0→t)估算的兰索拉唑片相对生物利用度为(99.9±15.9)%。结论用HPLC法测定血浆中兰索拉唑浓度,杂质无干扰,定量限低,重复性好,准确度高。受试的兰索拉唑片与参比的兰索拉唑片生物等效。

Aim To study the pharmacokinetics of lansoprazole tablets in human plasma. Methods Nineteen volunteers were given the lansoprazole tablets by oral administration with 2-way crossover design. The concentration of lansoprazole in plasma was determined by HPLC while the pharmacokinetic parameters were calculated by DAS software. Results The calibration curve was linear in the range from 20ng.mL^-1 to 2 000ng·mL^-1. The relative recovery was more than 95.14%. The intra and inter-day RSD was below 13.2%. The main pharmacokinetic parameters t1/2 , Cmax ,Tmax and AUC0→t for the test preparations were（2.24 ±0.89）h, （818.0 ±275.2） ng·mL^-1, （2.45 ± 0.47 ） h and （2 405 ± 1 141 ） ng·h·mL^ -1, respectively. Those for the reference preparations were （2.18 ± 0.85 ） h, （859.3 ±311.3）ng·mL^-1 , （2.45 ±0.47 ） h and （2 511 ± 1 351 ） ng·h·mL^-1 ,respectively. The relative bioavalability of the test preparations was （99.9 ± 15.9）%. Conclusion The HPLC method for determination of lansoprazole in plasma proved to be sensitive accurate and convenient. The reference and test preparations are bioequivalent.